详情描述
SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis.
Product information
Molecular Weight: 420.31
Formula: C16H19Cl2N3O4S
Chemical Name: (E)-3-(3,4-dichlorophenyl)-N-(2-(4-(methylsulfonyl)piperazin-1-yl)-2-oxoethyl)acrylamide
Smiles: CS(=O)(=O)N1CCN(CC1)C(=O)CNC(=O)/C=C/C1=CC(Cl)=C(Cl)C=C1
InChiKey: WUJBXFXHDUVSFM-HWKANZROSA-N
InChi: InChI=1S/C16H19Cl2N3O4S/c1-26(24,25)21-8-6-20(7-9-21)16(23)11-19-15(22)5-3-12-2-4-13(17)14(18)10-12/h2-5,10H,6-9,11H2,1H3,(H,19,22)/b5-3+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO 84 mg/mL (199.85 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Treatment with SR18662 significantly reduces growth and proliferation of CRC cells. SR18662 shows improved efficacy in reducing viability of multiple CRC cell lines. Flow cytometry analysis following SR18662 treatment shows an increase in cells captured in either S or G2/M phases of the cell cycle and a significant increase in the number of apoptotic cells. SR18662 treatment also reduces the expression of cyclins and components of MAPK and WNT signaling pathways.
In Vivo:
A significant dose-dependent inhibition of xenograft growth in mice is observed following SR18662 treatment that exceeds the effect of ML264 at equivalent doses. SR18662 is potential for colorectal cancer therapy.
References:
- Julie Kim, et al. Mol Cancer Ther. 2019 Nov;18(11):1973-1984.
Products are for research use only. Not for human use.